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5 Decades of Anti Histamines My Article Goo For Web Site
5 Decades of Anti Histamines My Article Goo For Web Site
Preface
But fortunately, all the available H1 blockers can be conveniently classified into several
classes. It would seem wise for the physician to get familiar with a few representative
compounds from the different classes and to base his choice on this knowledge.
Introduction
Histamine inhibitors
In 1910, Dale and Laidlaw discovered histamine. After the discovery of histamine, thirty
six long years had to be spent in painstaking research before a compound to block its
action could be found. But this phenolic ether amine was never used in humans
because it was too toxic. Another seven years had to pass before the first clinically
useful anti histamine, Pyrilamine could be synthesized. Soon, several compounds made
their appearance. They are now collectively called the first generation anti histamines.
They were all lipid-soluble and consequently crossed the blood-brain barrier – resulting
in sedation. Some have the unsavoury side effect of producing neural stimulation also,
leading to tremulousness. Even convulsions can result with supra therapeutic doses. In
the last 15 years, newer methods of synthesis led to the development of less lipophillic
antihistamines. Consequently, they are less liable to reach the brain and thus less liable
to produce sedation. These were called second generation antihistamines. Inspite of
their side effects, several first generation antihistamines are still usefully employed for
specific indications (Table1).
Clinical considerations
The Antihistamines are competitive inhibitors of histaminic action, either at the H1 or the
H2 receptor sites. They prevent the action of histamines, rather than reverse it. Hence
they are better given before histamine liberation occurs i.e. before the antigen challenge
occurs. Despite claims to the contrary, as a class, they lead to some degree of dry
mouth, sedation, lassitude and gastro intestinal symptoms. In a clinical situation when a
patient presents to you with signs of severe allergy, the drug of choice is adrenaline a
potent physiological antagonist of histamine. Further, several antihistamines do not
block the production of late phase mediators. This is why sometimes we need drugs
other than antihistamines like steroids (Table 2).
In table 3, the salient properties are indicated. Briefly put, all new antihistamines except
cetirizine,are less sedating. Terfenadine has a potential to lead to cardiac arrhythmia.
Loratidine can be given once a day. In view of the diurnal variation of the inhalational
allergy, this antihistamine can usefully be given in the night, so that it can cover the
early morning period.
Drug
Diphenhydramine
Cyclizine
Hydroxycine
Promethazine
Chlorcyclizine
Triplennamine
Azelastine